Cholestrol Lowering Drugs

Question 1

Statins MoA?

Answer 1

Inhibit HMG-CoA reductase

Decreases cholesterol synthesis in hepatocytes

Question 2

Statins ADRs?

Answer 2

Increased transaminase
Myopathy 
GI complaints
Arthralgias
Headaches

Question 3

Statins secondary benefits?

Answer 3

Anti-inflammatory
Decrease plaques
Decrease thrombotic risk
Increase endothelial cell function

Question 4

Fibric acid derivatives MoA?

Answer 4

PPAR-alpha agonist
Increases lipoprotein lipase production
Decreases TAG production
Increases fatty acid uptake

Question 5

Fibric acid derivatives ADR’s and contra-indications?

Answer 5

GI upset
Cholelithiasis
Myosotis
Abnormal LFTs
Don’t use in hepatic or renal dysfunction or pre-existing gallbladder disease

Question 6

Nicotinic acid MoA?

Answer 6

Inhibition of lipoprotein a synthesis

Decreases VLDL and increases HDL

Question 7

Nicotinic acid ADRs and contra-indications?

Answer 7

Flushing
Itching
Headache
Don’t use in liver disease due to hepatotoxicity
Don’t use if peptic ulcer history as can activate peptic ulcers

Question 8

Ezetimibe MoA?

Answer 8

Selectively inhibits intestinal cholesterol absorption
Decreases intestinal cholesterol delivery to liver
Increase hepatic LDL receptors
Decreases content of atherogenic particles
Drug and active metabolite circulates enterohepatcially and so delivers itself back to site of action (decreases systemic exposure)

Question 9

Ezetimibe ADRs?

Answer 9

Headache
Abdominal pain
Diarrhoea

Question 10

Fibrate and statin combination therapy actions and ADRS?

Answer 10

Decreases TAGs and LDLS
Increases HDL
Associated with increased myopathy and rhabdomyolosis risk
Don’t use Gemfibrozil (impairs statins), Fenofibrate impairs statins the least

Question 11

PC5K-9 Inhibitors MoA and example?

Answer 11

Evolocumab - Monoclonal antibody that inhibits proprotein convertase subtilisin kexin type 9

Question 12

What are PC5K9 Inhibitors used for?

Answer 12

Primary hypercholesterolaemia

Mixed dyslipidaemia